申请人:Shionogi & Co., Ltd.
公开号:US04476133A1
公开(公告)日:1984-10-09
4,1-Benzoxazepines of the following formula are novel central nervous system: ##STR1## wherein R is hydrogen or C.sub.1 to C.sub.5 alkyl; X is hydrogen, halogen, or nitro; Y is phenyl, 2-halophenyl, 4-halophenyl, 2-trifluoromethylphenyl, or pyridyl; and ##STR2## is a group of the formula: ##STR3## (wherein Q is oxygen, sulfur, or hydrazono, with a proviso that, when Y is phenyl or 2-halophenyl and R is hydrogen, Q is neither oxygen nor sulfur; R.sup.1 is hydrogen, halogen, C.sub.1 to C.sub.5 alkyl, C.sub.1 to C.sub.5 alkylthio, 5- or 6-membered heterocycle or C.sub.1 to C.sub.5 alkyl substituted by a substituent selected from the group consisting of halogen, hydroxy, mercapto, C.sub.1 to C.sub.5 alkoxy, C.sub.1 to C.sub.5 alkanoyloxy, C.sub.1 to C.sub.5 alkylthio, C.sub.7 to C.sub.9 aralkyldithio, C.sub.2 to C.sub.10 dialkylamino, C.sub.3 to C.sub.15 dialkylaminoalkoxy, C.sub.3 to C.sub.15 dialkylaminoalkylthio, and 5- or 6-membered heterocycle; R.sup.2 is C.sub.1 to C.sub.5 alkyl; and R.sup.3 is C.sub.1 to C.sub.5 alkyl or C.sub.3 to C.sub.10 dialkylaminoalkyl; with a proviso that when R.sup.1 is C.sub.1 to C.sub.5 alkyl and R is hydrogen, Y is neither phenyl nor 2-halophenyl)
以下化学式所示的4,1-苯并噁唑啉是新型中枢神经系统药物:##STR1## 其中R为氢或C.sub.1到C.sub.5烷基;X为氢,卤素或硝基;Y为苯基,2-卤苯基,4-卤苯基,2-三氟甲基苯基或吡啶基;而##STR2##是以下公式的基团:##STR3## (其中Q为氧,硫或肼酰基,但当Y为苯基或2-卤苯基且R为氢时,Q既不是氧也不是硫;R.sup.1为氢,卤素,C.sub.1到C.sub.5烷基,C.sub.1到C.sub.5硫代烷基,5或6成员杂环或C.sub.1到C.sub.5烷基,其被从卤素,羟基,硫巴,C.sub.1到C.sub.5烷氧基,C.sub.1到C.sub.5烷基酰氧基,C.sub.1到C.sub.5硫代烷氧基,C.sub.7到C.sub.9芳基硫代烷氧基,C.sub.2到C.sub.10二烷基氨基,C.sub.3到C.sub.15二烷基氨基烷氧基,C.sub.3到C.sub.15二烷基氨基烷硫基或5或6成员杂环所选的取代基所取代;R.sup.2为C.sub.1到C.sub.5烷基;R.sup.3为C.sub.1到C.sub.5烷基或C.sub.3到C.sub.10二烷基氨基烷基;但当R.sup.1为C.sub.1到C.sub.5烷基且R为氢时,Y既不是苯基也不是2-卤苯基。